1-[1-[(1-Methylindol-3-yl)methyl]piperidin-4-yl]-2-pyrrolidin-3-ylbenzimidazole

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: 1-[1-[(1-Methylindol-3-yl)methyl]piperidin-4-yl]-2-pyrrolidin-3-ylbenzimidazole
• 英文别名: 1-[1-[(1-methylindol-3-yl)methyl]piperidin-4-yl]-2-pyrrolidin-3-ylbenzimidazole
• 化学式: C₂₆H₃₁N₅
• 分子量: 413.6
• InChiKey: FELSQFRUUMKWIX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.3
• 重原子数：
  31
• 可旋转键数：
  4
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.42
• 拓扑面积：
  38
• 氢给体数：
  1
• 氢受体数：
  3

文献信息

• [EN] SUBSTITUTED BENZIMIDAZOLES AS NOCICEPTIN RECEPTOR MODULATORS<br/>[FR] BENZIMIDAZOLES SUBSTITUÉS EN TANT QUE MODULATEURS D'UN RÉCEPTEUR DE NOCICEPTINE
  申请人：SCRIPPS RESEARCH INST

  公开号：WO2014153529A1

  公开（公告）日：2014-09-25

  The invention provides modulators of the nociceptin receptor (NOP), including both agonists and antagonists. A compound of the invention can be a selective modulator of NOP with respect to the μ- and κ- opioid receptors (MOP and KOP), thus providing a therapeutic method for the treatment of conditions wherein selective NOP modulation is medically indicated and MOP or KOP modulation may be less desirable. A compound of the invention can be a NOP full agonist, partial agonist, inverse agonist, positive or negative allosteric modulator, or a functionally biased agonist. A compound of the invention can be used for the treatment of an anxiety state, post-traumatic stress disorder, addictive disorders (including overuse of alcohol, tobacco, and drugs of abuse such as cocaine, amphetamines, and opitates), misregulated food intake and/or energy expenditure, cough, sleep disorders, migraine, pain, depression, or neurodegenerative disorders such as Parkinsons disease or Alzheimers disease.

  该发明提供了辅料受体（NOP）的调节剂，包括激动剂和拮抗剂。该发明的化合物可以是NOP的选择性调节剂，相对于μ-和κ-阿片受体（MOP和KOP），因此提供了一种治疗方法，用于治疗需要选择性NOP调节而MOP或KOP调节可能不太理想的疾病。该发明的化合物可以是NOP的全激动剂、部分激动剂、逆激动剂、正或负变构调节剂，或功能性偏向激动剂。该发明的化合物可用于治疗焦虑状态、创伤后应激障碍、成瘾性障碍（包括滥用酒精、烟草和可卡因、安非他明和阿片类等药物）、食物摄入和/或能量消耗失调、咳嗽、睡眠障碍、偏头痛、疼痛、抑郁症，或帕金森病或阿尔茨海默病等神经退行性疾病的治疗。
• SUBSTITUTED BENZIMIDAZOLES AS NOCICEPTIN RECEPTOR MODULATORS
  申请人：THE SCRIPPS RESEARCH INSTITUTE

  公开号：US20160052913A1

  公开（公告）日：2016-02-25

  The invention provides modulators of the nociceptin receptor (NOP), including both agonists and antagonists. A compound of the invention can be a selective modulator of NOP with respect to the μ- and κ-opioid receptors (MOP and KOP), thus providing a therapeutic method for the treatment of conditions wherein selective NOP modulation is medically indicated and MOP or KOP modulation may be less desirable. A compound of the invention can be a NOP full agonist, partial agonist, inverse agonist, positive or negative allosteric modulator, or a functionally biased agonist. A compound of the invention can be used for the treatment of an anxiety state, post-traumatic stress disorder, addictive disorders (including overuse of alcohol, tobacco, and drugs of abuse such as cocaine, amphetamines, and opitates), misregulated food intake and/or energy expenditure, cough, sleep disorders, grain, pain, depression, or neurodegenerative disorders such as Parkinsons disease or Alzheimers disease.

  本发明提供了诺西普针受体(NOP)的调节剂，包括激动剂和拮抗剂。本发明的化合物可以是NOP的选择性调节剂，相对于μ-和κ-阿片受体(MOP和KOP)，从而为治疗选择性NOP调节在医学上指示和MOP或KOP调节可能不太理想的情况提供治疗方法。本发明的化合物可以是NOP的全激动剂、部分激动剂、反向激动剂、正或负的变构调节剂，或功能偏向激动剂。本发明的化合物可用于治疗焦虑状态、创伤后应激障碍、成瘾性障碍(包括滥用酒精、烟草和滥用药物，如可卡因、安非他命和阿片类药物)、不当的食物摄入和/或能量消耗、咳嗽、睡眠障碍、谷物、疼痛、抑郁症或神经退行性疾病，如帕金森病或阿尔茨海默病的治疗。
• US9656994B2
  申请人：——

  公开号：US9656994B2

  公开（公告）日：2017-05-23